Synthesis and Evaluation of Artemisinin-Based Hybrid and Dimer Derivatives as Antimelanoma Agents

青蒿素基杂化物和二聚体衍生物作为抗黑色素瘤药物的合成及评价

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作者:Lorenzo Botta, Silvia Filippi, Bruno M Bizzarri, Claudio Zippilli, Roberta Meschini, Rebecca Pogni, Maria Camilla Baratto, Luciano Villanova, Raffaele Saladino

Abstract

A library of hybrid and dimer compounds based on the natural scaffold of artemisinin was synthesized. These derivatives were obtained by coupling of artemisinin derivatives, artesunate, and dihydroartemisinin with a panel of phytochemical compounds. The novel artemisinin-based hybrids and dimers were evaluated for their anticancer activity on a cervical cancer cell line (HeLa) and on three complementary metastatic melanoma cancer cell lines (SK-MEL3, SK-MEL24, and RPMI-7951). Two hybrid compounds obtained by coupling of artesunate with eugenol and tyrosol, and one of the dimer compounds containing curcumin, emerged as the most active and cancer-selective derivatives.

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